ION CHANNEL MODULATING COMPOUNDS AND USES THEREOF - Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia.

2011-08-25

20110207731

SUBSTITUTED 4-(INDAZOLYL)-1,4-DIHYDROPYRIDINES AND METHODS OF USE THEREOF - This invention relates to novel 4-(indazolyl)-1,4-dihydropyridine og the following formula (I) derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.

PYRIMIDINE DERIVATIVES FOR TREATMENT OF ALZHEIMER'S DISEASE - The invention encompasses pyrimidine derivatives as gamma secretase modulators, useful for treating diseases associated with the deposition of beta-amyloid peptide in the brain, such as Alzheimer's disease, or of preventing or delaying the onset of dementia associated with such diseases. Pharmaceutical compositions and methods of use are included.

2011-08-25

20110207734

Azine Derivatives and Methods of Use Thereof - The present invention relates to Azine Derivatives, pharmaceutical compositions comprising the Azine Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.

2011-08-25

20110207735

CYANOPYRIMIDINONES - The invention relates to novel cyanopyrimidinones, process for their preparation, and the use thereof for producing medicaments for improving perception, concentration, learning and/or memory.

SUBSTITUTED BICYCLIC AMINES FOR THE TREATMENT OF DIABETES - Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.

2011-08-25

20110207738

ANNELATED PYRROLIDIN SULFONAMIDES WITH OXADIAZOLONE HEADGROUP, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS - The invention relates to annelated pyrrolidin sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula (I), in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

Activation of the Renin-Angiotensin System (RAS) and Sudden Cardiac Death - Provided herein are methods of treating a medical condition in which RAS activation is increased. The method comprises the step of administering to a subject a c-Src inhibitor in an amount effective to treat the medical condition. The invention also provides a method of treating or preventing a cardiac arrhythmia. The method comprises the step of administering to the subject a c-Src inhibitor in an amount effective to treat or prevent the cardiac arrhythmia. The invention additionally provides a method of delaying the onset of sudden cardiac death. The method comprises the step of administering to the subject a c-Src inhibitor in an amount effective to delay the onset of SCD. Methods of augmenting gap junction function and methods of increasing Connexin 43 levels in a subject in need thereof are further provided.

2011-08-25

20110207742

METHOD FOR REDUCTION, STABILIZATION AND PREVENTION OF RUPTURE OF LIPID RICH PLAQUE - There is to provide is an agent for reduction of a lipid rich plaque, stabilization of a lipid rich plaque and/or prevention of rupture of a lipid rich plaque in an atherosclerotic lesion comprising an effective amount of 2-[4-[2-(benzimidazole-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-p yridyl]acetamide (hereinafter, referred to as compound 1), its pharmaceutically acceptable salt or a hydrate thereof and Pitavastatin, and a pharmaceutically acceptable carrier, wherein the agent is intended to be simultaneously administered, or separately administered with interval of time to a patient in need thereof There is also to provide a method for reduction of a lipid rich plaque, stabilization of a lipid rich plaque and/or prevention of rupture of a lipid rich plaque in an atherosclerotic lesion, comprising simultaneously administering, or separately administering with interval of time an effective amount of the compound 1, its pharmaceutically acceptable salt or a hydrate thereof and an effective amount of Pitavastatin to a patient in need thereof.

Method for treating cognitive deficits - The invention relates to methods of treating cognitive dysfunction and improving cognitive functioning comprising the administration of trans-4-((1R,3S)-6-chloro-3-phenylindan-1-yl)-1,2,2-trimethylpiperazine or a pharmaceutically acceptable salt thereof to a patient in need thereof. Moreover the invention relates to an improved binder in a composition comprising 4-((1R,3S)-6-chloro-3-phenylindan-1-yl)-1,2,2-trimethylpiperazine.

NEW COMPOUNDS I - The present invention relates to compounds of formula (I),

2011-08-25

20110207747

2,5-Disubstituted Phenyl Carboxamide Orexin Receptor Antagonists - The present invention is directed to 2,5-disubstituted phenyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

BENZIMIDAZOLE AND AZA-BENZIMIDAZOLE CARBOXAMIDES - This invention provides compounds of Formula I which are PAFR antagonists: I and the pharmaceutically acceptable salts thereof. The compounds are useful for treating PAF-mediated disorders, and can be used in methods for treating atherosclerosis and preventing or reducing risk for atherosclerotic disease events. The compounds are also useful for treating or ameliorating pain, e.g. inflammatory pain and/or nociceptive pain, and for treating or ameliorating autoimmune and/or inflammatory diseases, among other conditions.

2011-08-25

20110207751

HETEROCYCLIC COMPOUNDS AND USES AS ANTICANCER AGENTS - Novel compounds having a fused bicyclic heteroaromatic ring system substituted with a thiazole ring are disclosed. The compounds inhibit growth of a variety of types of cancer cells, and are thus useful for treating cancer. Efficacy of these compounds is demonstrated with a system for monitoring cell growth/migration, which shows they are potent inhibitors of growth and/or migration of cancer cells. In addition, compounds of the invention were shown to stop growth of tumors in vivo, and to reduce the size of tumors in vivo. Compositions comprising these compounds, and methods to use these compounds and compositions for treatment of cancers, are disclosed.

METHODS FOR TREATING PAIN - The present invention features methods and compositions for preventing, reducing, or treating a traumatic, metabolic or toxic peripheral nerve lesion or pain including, for example, neuropathic pain, inflammatory and nociceptive pain by administering to a mammal in need thereof a compound that reduces the expression or activity of BH4. According to this invention, this reduction may be achieved by reducing the enzyme activity of any of the BH4 synthetic enzymes, such as GTP cyclohydrolase (GTPCH), sepiapterin reductase (SPR), or dihydropteridine reductase (DHPR); by antagonizing the cofactor function of BH4 on BH4-dependent enzymes; or by blocking BH4 binding to membrane bound receptors. The compounds of the invention may be administered alone or in combination with a second therapeutic agent.

2011-08-25

20110207754

CYCLOBUTANE AND METHYLCYCLOBUTANE DERIVATIVES AS JANUS KINASE INHIBITORS - The present invention relates to cyclobutane and methylcyclobutane derivatives, as well as their salts, compositions, and methods of use, which are Janus kinase (JAK) inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer and myeloproliferative disorders.

Tricyclic Compounds Having Cytostatic and/or Cytoxic Activity and Methods of Use Thereof - The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.

2011-08-25

20110207758

Methods for Therapeutic Renal Denervation - Methods for therapeutic renal denervation are disclosed herein. One aspect of the present application, for example, is directed to methods that block, reduce and/or inhibit renal sympathetic nerve activity to achieve a reduction in central sympathetic tone. Renal sympathetic nerve activity may be altered or modulated along the afferent and/or efferent pathway. The achieved reduction in central sympathetic tone may carry several therapeutic benefits across many disease states.

2011-08-25

20110207759

METHOD FOR TREATMENT OF ATHEROSCLEROTIC DISEASE - A method of effecting regression of atherosclerotic disease in a patient whose plasma lipid concentrations are at levels considered normal or optimal. The method involves treating the patient with a combination of a 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitor and niacin. Disease regression has been observed over periods as short as 14 months, preferably 8 months.

2011-08-25

20110207760

SN-38 COMPOSITIONS - In one aspect, the present invention is directed to a stable aqueous composition including (a) SN-38; (b) a sulfoalkyl derivative of a cyclodextrin; and (c) water; in which the concentration of SN-38 in the composition is at least about 0.13 mg/g of the composition. In another aspect, this invention is directed to a process for making the composition which process comprises mixing SN-38 and a sulfoalkyl derivative of a cyclodextrin in an aqueous medium wherein the water content of the mixture is less than about 60% by weight.

2011-08-25

20110207761

Diversion- and/or abuse-resistant aompositions and methods for making the same - A composition formulated for diversion- and/or abuse-resistance, includes at least one active pharmaceutical ingredient (API), each present in an acidic form, a first compound capable of coupling to the acidic form of the API to form a complex, where the resulting complex is resistant to separation by conventional separation methods, and a second compound capable of preferentially coupling to the first compound to thereby release the API from the complex.

CYCLOPOLYSACCHARIDE COMPOSITIONS - The present invention is directed to a composition including: (a) an active ingredient other than bendamustine; (b) a charged cyclopolysaccharide comprising at least one charged group; and (c) a stabilizing agent comprising at least one charged group having a charge opposite to that of the cyclopolysaccharide. The composition provides unexpectedly desirable stability in reactive environments such as plasma which contain entities (such as enzymes, other proteins and the like) and/or conditions which can decompose or deactivate the active ingredient.

2011-08-25

20110207765

TOPICAL COMPOSITION COMPRISING A COMBINATION OF AT LEAST TWO PENETRATION ENHANCING AGENTS - The present invention relates to a composition for improved transdermal drug delivery comprising a drug, a combination of at least two penetration enhancing agents, wherein at least one of the penetration enhancing agents is selected from the group consisting of esters of saturated or unsaturated fatty acids and lower alcohols, and iso-form alcohols; wherein at least one of the penetration enhancing agents is selected from the group consisting of aliphatic diols and triols; and wherein the components are present in a non-aqueous solvent system. A preferred topical composition comprises the active substance imiquimod and the penetration enhancing agents isopropyl myristate and propylene glycol.

2011-08-25

20110207766

LOWER DOSAGE STRENGTH IMIQUIMOD FORMULATIONS AND SHORT DOSING REGIMENS FOR TREATING GENITAL AND PERIANAL WARTS - Pharmaceutical formulations and methods for the topical or transdermal delivery of 1isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5 c]quinolin-4-amine, i.e., imiquimod, to treat genital/perianal warts with shorter durations of therapy than currently prescribed for the commercially available Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating genital/perianal warts with an acceptable safety profile and dosing regimens that are shorter and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara® 5% imiquimod cream to treat genital/perianal warts are also disclosed and described.

2011-08-25

20110207767

Novel cc-1065 Analogs and Their Conjugates - This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.

2011-08-25

20110207768

PHARMACEUTICAL COMBINATION OF ANTIBACTERIAL AND ANTIFUNGAL CREAM - A method for the emperic treatment of an intertrigal skin infection potentially caused by a gram-positive bacteria in a human patient that includes a topical administration to the patient of a pharmaceutical formulation comprising a bactericidal amount of a Gram-positive bactericide and an antimycotic amount of an antifungal component suspended in a skin-barrier carrier.

PHARMACEUTICAL PRODUCT COMPRISING A MUSCARINIC RECEPTOR ANTAGONIST AND A SECOND ACTIVE INGREDIENT - The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is a selected muscarinic receptor antagonist, and a second active ingredient which is selected from a phosphodiesterase inhibitor, a modulator of chemokine receptor function, an inhibitor of kinase function, a protease inhibitor, a steroidal glucocorticoid receptor agonist, a non-steroidal glucocorticoid receptor agonist and a purinoceptor antagonist, of use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease and asthma.

NOVEL PHENYL-QUINOLINE-CARBOXYLIC ACID PYRIDINE DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS - This invention relates to novel phenyl-quinoline-carboxylic acid pyridine derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

2011-08-25

20110207774

TRIAZOLOTHIADIAZOLE INHIBITOR OF C-MET PROTEIN KINASE - The present invention relates to compound 1, which is useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising Compound 1 and methods of using the compositions in the treatment of proliferative disorders.

2011-08-25

20110207775

AGENT THAT MODULATES PHYSIOLOGICAL CONDITION OF PESTS, INVOLVED IN INSECT VESICLE-FUSING ATPASE ACTIVITY - The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect vesicle-fusing ATPase; a method for assaying pesticidal activity of a test substance, which comprises measuring the activity of a vesicle-fusing ATPase in a reaction system in which the vesicle-fusing ATPase contacts with a test substance, and the like.

2011-08-25

20110207776

Use of D4 and 5-HT2A antagonists, inverse agonists or partial agonists - The present invention relates to the use of compounds and compositions of compounds having D4 and 5-HT2A antagonistic, partial agonistic or inverse agonistic activity for the treatment of the underlying dysregulation of the emotional functionality of mental disorders (i.e. affect instability—hypersensitivity—hyperaesthesia—dissociative phenomena—etc). The invention also relates to methods comprising administering to a patient diagnosed as having a neuropsychiatric disorder a pharmaceutical composition containing (i) compounds having D4 antagonistic, partial agonistic or inverse agonistic activity and (ii) compounds having 5-HT2A antagonistic, partial agonistic or inverse agonistic, and (iii) any known medicinal compound and compositions of said compounds. The combined D4 and 5-HT2A antagonistic, partial agonistic or inverse agonistic effects may reside within the same chemical or biological compound or in two different chemical and/or biological compounds.

PROCESS FOR THE PREPARATION OF ESOMEPRAZOLE MAGNESIUM - The present invention relates to a process for the preparation of esomeprazole magnesium containing R-isomer greater than about 0.1% by wt. In particular, the present invention relates to a process for the preparation of esomeprazole magnesium dihydrate containing R-isomer greater than about 0.1% by wt.

NOVEL MICROBIOCIDES - Compounds of Formula (I), in which the substituents are as defined in claim

2011-08-25

20110207782

NICOTINE-CONTAINING PRODUCT - A nicotine-containing product comprising a pharmaceutically acceptable polymeric substrate, which is able to bind cations, nicotine or a pharmaceutically acceptable nicotine derivative, and pharmaceutically acceptable inorganic cations. It further pertains to a method for the preparation of such a nicotine-containing product and to the use thereof for the preparation of a pharmaceutical product.

2-Aryl-Propionic Acids and Derivatives and Pharmaceutical Compositions Containing Them - The present invention relates to (R,S) 2-aryl-propionic acids and derivatives, their single enantiomer (S) and to pharmaceutical compositions containing them, which are used in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonucleated neutrophils (PIvTN leukocytes) at inflammation sites. The present invention provides compounds for use in the treatment of transient cerebral ischemia, bullous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and damages caused by ischemia and reperfusion. (Formula (I)

2011-08-25

20110207786

Potentiated Biocidal Compositions and Methods of Use - The present technology relates to biocidal compositions and methods that contain and utilize at least one biocidal agent and at least one potentiator system wherein the resultant combination has an enhanced biocidal efficacy. The present technology also discloses a rapid screening assay for determining biocidal compositions with enhanced efficacy, e.g., a microbial contact kill time of 5 minutes or less. Further, the present technology provides a method of determining biocidally effective concentrations of biocidal compositions comprising at least one biocidal agent and at least one potentiator system.

2011-08-25

20110207787

ANTIMICROBIAL COMPOSITIONS - What is described herein are antimicrobial compositions which are defined blends of a 1,2-diol and phenoxyethanol which show broad activity against bacteria, fungi and mold spores. This activity is potentiated by the addition thereto of small amounts of a co-biocide for which the blend acts as a delivery system for the otherwise water-insoluble co-biocide.

PHARMACEUTICAL COMPOSITION - The present invention relates to an oral controlled release pharmaceutical composition in the form of a unit dosage form comprising:

2011-08-25

20110207795

SMAD7 INHIBITOR COMPOSITIONS AND USES THEREOF - The present invention relates to the use of a specific inhibitor of Smad7 expression or function for the preparation of a pharmaceutical composition for the prevention, amelioration or treatment of a disease of the central nervous system and/or diseases related and/or caused by said disease of the central nervous system. Furthermore, methods for preventing, ameliorating and/or treating such diseases are disclosed.

2011-08-25

20110207796

ALPHA-SYNUCLEIN KINASE - Agents and methods for treatment of diseases associated with Lewy body diseases (LBDs) in the brain of a patient are provided. Preferred agents include inhibitors of PLK2 kinase.

2011-08-25

20110207797

ENHANCED ANTISENSE OLIGONUCLEOTIDES - Described herein are gap-widened antisense oligonucleotides having improved therapeutic index as compared to 5-10-5 MOE gapmer antisense oligonucleotides of the same sequence. Also described are methods of reducing a target RNA in an animal using the gap-widened antisense oligonucleotides of the present invention. Further, are methods for selecting a gap-widened antisense oligonucleotides.

Compositions for Targeted Delivery of siRNA - The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted delivery polymers. Delivery polymers provide membrane penetration function for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness to the delivery polymers.

2011-08-25

20110207800

HIV-Dependent expression constructs and uses therefore - The invention provides a nucleic acid construct for targeting and killing cells infected with the human immunodeficiency virus (HIV). The construct includes an HIV Tat-dependent promoter operably linked to the coding region for a cell-killing protein, such as anthrolysin-O (anlO), which is partially or fully within an intron defined by a splice donor site and a splice acceptor site. The construct further includes a Rev Responsive Element (RRE). Therapeutic methods of treating HIV infection are also provided.

2011-08-25

20110207801

Novel Genes, Compositions, and Methods for Modulating the Unfolded Protein Response - The present invention relates to methods and compositions for modulating the unfolded protein response. The method further relates to methods and compositions for the treatment and diagnosis of protein conformational diseases or disorders, including, but not limited to, α1-antitrypsin deficiency, cystic fibrosis, and autoimmune diseases and disorders. The invention further provides methods for modulating the unfolded protein response by modulating XBP1 mRNA splicing.

2011-08-25

20110207802

GLUTAMIC ACID DECARBOXYLASE (GAD) BASED DELIVERY SYSTEM - The invention provide methods and compositions for localized delivery of a vector comprising a therapeutic agent to a specific region of the brain that is overstimulated in neurodegenerative diseases. In particular, the invention provides methods and compositions used to deliver an adeno-associated virus vector (AAV) comprising a nucleotide sequence encoding glutamic acid decarboxylase (GAD) to cells in the hippocampus, subthalamic nucleus of the basal ganglia, mesaphilia and thalamus.

2011-08-25

20110207803

Taxane Pro-Emulsion Formulations and Methods Making and Using the Same - Taxane pro-emulsion formulations are provided. Pro-emulsion formulations are dried powders that include a taxane, oil, surfactant and sugar alcohol. Also provided are methods of making and using the pro-emulsion formulations, as well as kits that include the pro-emulsion formulations.

2011-08-25

20110207804

COMPOSITIONS FOR THE TREATMENT OF NEOPLASTIC DISEASES - Solid pharmaceutical taxane compositions for oral administration which comprise a substantially amorphous taxane, a carrier, and a surfactant, wherein the substantially amorphous taxane is prepared by a solvent evaporation method, such as spray drying. Methods of preparation of the composition and uses of the composition also are included.

FORMULATION OF DUAL CYCLOXYGENASE (COX) AND LIPOXYGENASE (LOX) INHIBITORS FOR MAMMAL SKIN CARE - The present invention provides a novel composition of matter comprised of a mixture of two specific classes of compounds—Free-B-Ring flavonoids and flavans—for use in the prevention and treatment of diseases and conditions associated with the skin. This composition of matter simultaneously inhibits cyclooxygenase (COX) and lipoxygenase (LOX) enzymatic activity in normal, aged and damaged dermal cells and tissues. This invention further provides a method for the prevention and treatment of diseases and conditions of the skin mediated by cyclooxygenase (COX) and lipoxygenase (LOX). The method for preventing and treating COX and LOX mediated diseases and conditions of the skin is comprised of topically administering to a host in need thereof a therapeutically effective amount of a composition comprising a mixture of Free-B-Ring flavonoids and flavans synthesized and/or isolated from a single plant or multiple plants, preferably in the

2011-08-25

20110207807

NEW USE FOR HOMOISOFLAVONE OR A SALT THEREOF - The present disclosure relates to a new use of homoisoflavanone or a salt thereof. More particularly, it relates to a pharmaceutical composition for the prevention and treatment of inflammatory diseases or allergic diseases comprising homoisoflavanone represented by Chemical Formula 1 or a salt thereof, a use of homoisoflavanone or a salt thereof in the manufacture of an agent for the preventing and treating of inflammatory diseases or allergic diseases, and a method for treating inflammatory diseases or allergic diseases including administering an effective dose of homoisoflavanone or a salt thereof to a subject in need thereof.

N1-BENZO[1,3]DIOXOL-5-YLMETHYL-N2-SUBSTITUTED BIGUANIDE DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME - The present invention provides an N1-benzo[1,3]dioxol-5-ylmethyl-N2-substituted biguanide derivative of formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing same, and a pharmaceutical composition comprising same as an active ingredient. The inventive N1-benzo[1,3]dioxol-5-ylmethyl-N2-substituted biguanide derivative exhibits improved blood glucose level- and lipid level-lowering effects even with a reduced dosage as compared to conventional drugs, and thus, it is useful for preventing or treating diabetes, metabolic syndromes such as insulin-independent diabetes, obesity and atherosclerosis, or a P53 gene defect-related cancer.

PHARMACEUTICAL COMPOSITION WITH GELLING PROPERTIES CONTAINING A TYROSINE DERIVATIVE - The present invention relates to an injectable pharmaceutical composition with gelling properties containing:—an active principle; a hydrophobic and bio-compatible organic liquid; and an organogelling substance, the molecules of which have the capacity to bind together via bonds of low energy, wherein said organogelling substance is chosen among L-tyrosine derivatives responding to the following formula (I) wherein: R1 is an alkyl group containing 1 to 3 carbon atoms, linear or branched; and R2 is a hydrophobic group chosen among aliphatic saturated or unsaturated fatty chains or aryl or arylalkyl groups, Its use as a vector for the release of active principles, as well as its process of preparation.

2011-08-25

20110207814

Combination Therapy for Breast Cancer Treatment - The present invention provides a novel treatment which features immune therapy in the context of the functions of MSCs as a novel approach to breast cancer treatment. By identifying and elucidating the role of MSCs in the behavior of breast cancer cells at metastatic sites and also at the primary region, this invention provides novel approaches for therapeutic intervention. More particularly, in the presence of MSCs a CXCR4 antagonist transitioned BCCs into cycling cells and conferred susceptibility to a chemotherapeutic agent. The proliferation of BCCs depended on the release of IL-1α and IL-1β from MSCs, but only if the CXCR4 antagonist uncoupled BCCs from MSCs.

ALTERNATE MORPHEEINS OF ALLOSTERIC PROTEINS AS A TARGET FOR THE DEVELOPMENT OF BIOACTIVE MOLECULES - A composition having an agent adapted to affect a multimeric protein by binding to a binding site of the multimeric protein and thereby affecting an equilibrium of units, wherein the multimeric protein has an assembly having a plurality of said units, wherein each of the units has a first complementary surface and a second complementary surface and wherein the first complementary surface of one unit is associated with the second complementary surface of another unit, provided that the assembly is at least one of different quaternary isoforms on a condition that in the multimeric protein (1) a structure of each of the units determines a structure of the different quaternary isoforms, (2) the units are in the equilibrium and (3) the structure of the different quaternary isoforms influences a function of the multimeric protein.

DISINFECTING AND ANTIMICROBIAL COMPOSITIONS - Broad spectrum disinfecting and microbicidal compositions of biodegradable and environmentally friendly compositions containing esters formed from fatty organic alcohols and fatty carboxylic acids. These compositions display activities against the most resistant microbial forms including bacterial spores. The preparations can be used in health care, food processing, personal care and other industries where the use of harsh oxidizing chemicals is undesirable.

2011-08-25

20110207819

Fat Emulsion for Artificially Feeding Seriously Ill Intensive Care Patients - The present invention relates to a pharmaceutical preparation for the prophylaxis and treatment of critical illness polyneuropathy (CIP) and critical illness myopathy (CIM). The invention further relates to an isotonic fat emulsion comprising at least one triglyceride that comprises at least one fatty acid group having an odd number of carbon atoms, wherein the fatty acid group comprises a carbon chain having 5 to 15 carbon atoms.

12-HOUR SUSTAINED-RELEASE METOCLOPRAMIDE - The present invention consists of an extended-release metoclopramide hydrochloride pharmaceutical composition, in 15 mg drug substance tablets, for use in gastrointestinal disorders. The formulation is mainly composed of a hydrophilic polymer, a hydrophobic polymer, a hydrophilic component and metoclopramide hydrochloride. The hydrophilic polymer is swollen by hydration when contacting water, forming a gel coat which controls drug substance release. The water inside the matrix dissolves the drug substance and this is diffused outside through the gel coat. The hydrophobic polymer shows plastic deformation properties under compression, tending to surround the drug substance particles reducing the pore quantity and dimensions in the matrix structure, delaying as a consequence the drug substance release. The hydrophilic component is part of the gel coating structure providing support thereto. Drug substance is the metoclopramide hydrochloride or a pharmaceutically acceptable salt thereof.

LACTOSE AND CELLULOSE-BASED TABLETING AID - The present invention concerns a process for producing a granulate based on lactose and cellulose (derivative), a granulate obtainable by the process and its use as a tabletting excipient.

2011-08-25

20110207827

METHOD FOR DETERMINING SENSITIVITY OR RESISTANCE TO COMPOUNDS THAT ACTIVATE THE BRAIN SEROTONIN SYSTEM - The invention relates to a method for determining whether a patient suffering from a condition that is susceptible to treatment with a compound that activates the brain serotonin system is susceptible or resistant to treatment with the compound. The method includes establishing whether the patient is a pre-adult, a transition age patient, or an adult and observing whether the genome of the patient contains at least one copy of a BDNF allele having a genetic alteration. The method further includes correlating the presence of the allele containing the genetic alteration with susceptibility or resistance of the patient to the treatment with the compound, wherein a pre-adult patient containing the genetic alteration is correlated as being susceptible to the treatment; a transition age patient containing the genetic alteration is correlated as being susceptible or resistant to the treatment; and an adult patient containing the genetic alteration is correlated as being resistant to the treatment.